Source text - EnglishOver the years, we've had an active program in the total and
semi-synthesis of antibiotics as well as in their chemical modification based on biological rationales.
Quantamycin, a computer-simulated inhibitor of ribosomal binding is an example of a successful, biologically inspired synthetic program (See topic 7).
Avermectin, a potent anthelmintic agent has been the target of total synthesis and chemical modification.
Other total syntheses of clinically important molecules include thienamycin, dihydromevinolin, ajmalicine, tetrahydrolipstatin, reserpine, among others.
A number of current research programs deal with the validation of biochemical hypotheses (mode of action, etc.) through rational design of models and novel drugs.
An active area of research involves the design of peptidomimetics, enzyme inhibitors, antagonists, novel β-lactams and β-lactamase inhibitors relying on structure-based design and available X-ray data.
Another area of current interest is the design and synthesis of RNA-binding molecules, including aminoglycoside antibiotics.